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Titolo:
SPECT imaging with the D-4 receptor antagonist L-750,667 in nonhuman primate brain
Autore:
Staley, JK; Tamagnan, G; Baldwin, RM; Fujita, M; Al Tikriti, MS; Eshima, L; Thornback, J; Roe, D; Lu, L; Seibyl, JP; Innis, RB;
Indirizzi:
Yale Univ, Sch Med, Dept Psychiat, W Haven, CT 06516 USA Yale Univ W Haven CT USA 06516 Med, Dept Psychiat, W Haven, CT 06516 USA Yale Univ, Sch Med, Dept Pharmacol, W Haven, CT 06516 USA Yale Univ W Haven CT USA 06516 Med, Dept Pharmacol, W Haven, CT 06516 USA Yale Univ, Sch Med, Dept Diagnost Radiol, W Haven, CT 06516 USA Yale UnivW Haven CT USA 06516 ept Diagnost Radiol, W Haven, CT 06516 USA VA Connecticut Healthcare Syst, W Haven, CT USA VA Connecticut Healthcare Syst W Haven CT USA care Syst, W Haven, CT USA Resolut Pharmaceut, Mississauga, ON, Canada Resolut Pharmaceut Mississauga ON Canada maceut, Mississauga, ON, Canada
Titolo Testata:
NUCLEAR MEDICINE AND BIOLOGY
fascicolo: 6, volume: 27, anno: 2000,
pagine: 547 - 556
SICI:
0969-8051(200008)27:6<547:SIWTDR>2.0.ZU;2-8
Fonte:
ISI
Lingua:
ENG
Soggetto:
DOPAMINE D4 RECEPTORS; HIGH-AFFINITY; PHARMACOLOGICAL CHARACTERIZATION; SELECTIVE ANTAGONIST; H-3 NEMONAPRIDE; MESSENGER-RNA; SCHIZOPHRENIA; RAT; STRIATUM; RADIOLIGAND;
Keywords:
dopamine D-4 receptor; L750,667; SPECT; primate brain;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
51
Recensione:
Indirizzi per estratti:
Indirizzo: Staley, JK Yale Univ, Sch Med, Dept Psychiat, 950 Campbell Ave, W Haven, CT 06516 USA Yale Univ 950 Campbell Ave W Haven CT USA 06516 n, CT 06516 USA
Citazione:
J.K. Staley et al., "SPECT imaging with the D-4 receptor antagonist L-750,667 in nonhuman primate brain", NUCL MED BI, 27(6), 2000, pp. 547-556

Abstract

The suitability of an I-123-labeled form of the putative D-4 receptor ligand L750,667 as a radiotracer for single photon emission computed tomographyimaging was assessed in nonhuman primates. [I-123]L750,667, labeled by iododestannylation, was administered to baboons in bolus and bolus plus constant infusion paradigms and imaged for 6 h. Total [I-123]L750,667 brain uptake peaked (2.3% injected dose) at 15 min postinjection. [I-123]L750,667 uptake was observed in all brain regions measured including diencephalon, brainstem, basal ganglia, cingulate cortex, and cerebellum, and slightly lower levels were noted in the frontal, parietal, temporoinsular, and occipital cortices. Administration of the D-4 receptor antagonist NGD 94-1 (2 mg/kg) did not displace radioactivity from any of the brain regions examined. Thus, while L750,667 is selective for the D-4 receptor in vitro, because brain [I-123]L750,667 uptake was not displaced by NGD 94-1 at receptor saturating doses, [I-123]L750,667 does not appear to be a suitable radiotracer for in vivo imaging of the D-4 receptor. NUCL MED BIOL 27;6:5411-556, 2000. (C) 2000 Elsevier Science Inc. All rights reserved.

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Documento generato il 21/01/20 alle ore 00:53:04